Precision-cut human liver slices are an important tool for defining the metabolism and hepatotoxicity of drug candidates early in development. Because of the frequent use of this in vitro tool, a knowledge of the catalytic activities of the drug-metabolizing enzymes during human liver slice culture is necessary. Therefore, marker catalytic activities for various cytochrome P450 (P450 or CYP) fo...

A series of 3-acylhydrazono-4-hydroxycoumarins were synthesized via condensation of 3-acetyl-4-hydroxycoumarin with appropriate hydrazides. The structures of the newly-synthesized compounds were characterized by spectral and elememental analysis or HRMS measurements. Their antioxidant properties were evaluated by using scavenging effects on 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical as well a...

Testosterone and 7-ethoxycoumarin were used as substrates to quantify the maintenance of phase I and II enzymes in precision-cut rat liver slices in dynamic organ culture. Testosterone hydroxylations, 7-ethoxycoumarin O-deethylation, 7-hydroxycoumarin sulfate, and 7-hydroxycoumarin glucuronide formation were all maintained at initial levels in the slice incubation media after incubation for up ...

A novel catalytic synthesis of 3,3'-(arylmethylene)-bis-(4-hydroxy-2H-chromene-2-one) derivatives from a tandem condensation reaction of 4-hydroxycoumarin and aromatic aldehydes has been developed. The reaction occurs in water in the presence of Melamine trisulfonic acid as catalyst to give the corresponding products in good to high yields. This green approach has several advantages such as sho...

The effect of starvation and glucose addition on glucuronidation was assessed in sublobular regions of the lobule in perfused livers from phenobarbital-treated rats. Fibre-optic micro-light guides were placed on periportal and pericentral areas on the surface of livers to monitor the fluorescence (excitation 366 nm, emission 450 nm) of free 7-hydroxycoumarin from the tissue surface. After infus...

Acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) are the key enzymes in pathogenesis of Alzheimer's disease (AD), which is characterized by a deficit in central cholinergic transmission. In the current study, AChE and BChE inhibitory activities of seven coumarin derivatives [umbelliferone (1), 4-methylumbelliferone (2), 4-hydroxycoumarin (3), scopoletin (4), 8-methoxypsoralen (5), b...